DNA polymerase beta (pol β) inhibitors: a comprehensive overview

Drug Discovery Today
Khaled BarakatJack Tuszynski

Abstract

Base excision repair (BER) is the fundamental pathway responsible for the elimination of damaged DNA bases and repair of DNA single-strand breaks generated spontaneously or produced by DNA-damaging agents. Among the essential enzymes that are required to achieve the BER reaction is DNA polymerase beta (pol β), which has been regarded as a potential therapeutic target. More than 60 pol β-inhibitors have been identified so far; however, most of them are either not potent or not specific enough to become a drug. In this article we compile an essential knowledge base regarding the structures, the modes of inhibition and the activities of these pharmacologically interesting molecules.

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Citations

Sep 26, 2012·Journal of Medicinal Chemistry·Malay PatraGilles Gasser
Sep 26, 2015·Journal of Molecular Graphics & Modelling·Summer KassemKhaled H Barakat
Feb 21, 2016·Pharmacology & Therapeutics·Navnath S GavandeJohn J Turchi
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Feb 28, 2015·Journal of Molecular Graphics & Modelling·Clement ViricelKhaled Barakat
Jul 1, 2016·Journal of Medicinal Chemistry·Dmitry M Korzhnev, M Kyle Hadden
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Aug 11, 2020·Bioorganic & Medicinal Chemistry·Sasha M DaskalovaSidney M Hecht
Jul 10, 2021·ACS Chemical Biology·Shelby C YuhasMarc M Greenberg
Jul 3, 2021·Chembiochem : a European Journal of Chemical Biology·Shelby C YuhasMarc M Greenberg

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